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Ronoprost, Ornoprostil, OU-1308, Ronok, Alloca

奥洛前列素Chemical Name: 17S,20-Dimethyl-6-oxoprostaglandin E1 methyl ester
CAS No. 70667-26-4
项目整合开发状态: Withdrawn
项目研究机构: Ono (Originator), Pfizer (Originator)
合成路线:The reaction of methyl 9alpha,11alpha,15(S)-trihydroxy-17(S),20-dimethylprosta-5(Z),13(E)-dienoate (I) with I2 and NaHCO3 in water dichloromethane gives the iodoepoxy compound (II),which is treated with dihydropyran-p-toluenesulfonic acid in dichloromethane to protect the hydroxyl groups yielding the bistetrahydropyranyl derivative (II).The dehydrohalogenation of (III) with 1,5-diazabicyclo[5.4.O]-5-undecene (DBU) followed by hydrolysis with HCl affords the hydroxyketone (IV),which is further oxidized with CrO3-MnSO4-H2SO4 to the diketone (V).Finally,this compound is deprotected with aqueous acetic acid in THF.
📌 参考资料/链接:
参考文献标题:Prostaglandin analogues
文献作者:Hayashi,M.; Arai,Y.; Shimoji,K.(Ono Pharmaceutical Co.,Ltd.; Pharmacia Corp.)
参考来源:DE 2840032

📄 详细内容


合成路线:The reaction of methyl 9alpha,11alpha,15(S)-trihydroxy-17(S),20-dimethylprosta-5(Z),13(E)-dienoate (I) with I2 and NaHCO3 in water dichloromethane gives the iodoepoxy compound (II),which is treated with dihydropyran-p-toluenesulfonic acid in dichloromethane to protect the hydroxyl groups yielding the bistetrahydropyranyl derivative (II).The dehydrohalogenation of (III) with 1,5-diazabicyclo[5.4.O]-5-undecene (DBU) followed by hydrolysis with HCl affords the hydroxyketone (IV),which is further oxidized with CrO3-MnSO4-H2SO4 to the diketone (V).Finally,this compound is deprotected with aqueous acetic acid in THF.

参考文献标题:Ornoprostil
文献作者:Castar,R.M.; Serradell,M.N.; Castar,J.
参考来源:Drugs Fut 1987,12(11),1023


合成路线:The reaction of methyl 9alpha,11alpha,15(S)-trihydroxy-17(S),20-dimethylprosta-5(Z),13(E)-dienoate (I) with I2 and NaHCO3 in water dichloromethane gives the iodoepoxy compound (II),which is treated with dihydropyran-p-toluenesulfonic acid in dichloromethane to protect the hydroxyl groups yielding the bistetrahydropyranyl derivative (II).The dehydrohalogenation of (III) with 1,5-diazabicyclo[5.4.O]-5-undecene (DBU) followed by hydrolysis with HCl affords the hydroxyketone (IV),which is further oxidized with CrO3-MnSO4-H2SO4 to the diketone (V).Finally,this compound is deprotected with aqueous acetic acid in THF.
参考文献标题:
文献作者:Suarez-Kurtz,G.; et al.
参考来源:Res Disclosure 1985,256(9),400-401


产品链接: CAS No. 70667-26-4››